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Vascular smooth muscle cell targets

Molecular classification
G protein-coupled receptor, Ion channel, Enzyme, Transcription factor, Receptor
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Overview

Vascular smooth muscle cell (VSMC) targets represent a broad category of molecular entities located on or within the smooth muscle cells of blood vessels that regulate vascular tone, blood pressure, and structural remodeling (StatPearls, 2023). These targets include various G protein-coupled receptors such as the Angiotensin II type 1 receptor and alpha-1 adrenergic receptors, as well as ion channels like L-type voltage-gated calcium channels (PubMed, PMID: 30135141). In healthy physiology, these targets mediate the contraction and relaxation of the vessel wall in response to neural and humoral stimuli. In pathological states such as hypertension, atherosclerosis, and pulmonary arterial hypertension, VSMCs undergo phenotypic switching from a contractile to a synthetic state, contributing to vessel narrowing and wall thickening (NIH, 2022). Pharmacological modulation of these targets is a cornerstone of cardiovascular medicine, utilizing agents like calcium channel blockers, ARBs, and vasodilators to manage systemic and pulmonary vascular resistance (PubChem). Because this term refers to a heterogeneous group of proteins rather than a single molecular entity, it is classified as a non-specific target category.

Other names
VSMC targetsVascular smooth muscle targetsVascular smooth muscle cell signaling molecules
02

Mechanism of action

Drugs targeting vascular smooth muscle cells act through various mechanisms including the blockade of L-type calcium channels, antagonism of G protein-coupled receptors (such as angiotensin II type 1 and endothelin receptors), and the activation of soluble guanylate cyclase to increase cyclic GMP levels.

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Biological functions

VasoconstrictionVasodilationCell proliferationCell migrationPhenotypic switching
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Disease associations

HypertensionAtherosclerosisRestenosisPulmonary arterial hypertensionAneurysm
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Safety considerations

Systemic hypotensionPeripheral edemaReflex tachycardiaElectrolyte disturbancesSyncope
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Interacting drugs

Amlodipine

5 more in the full profile.

07

Biomarkers

Alpha-smooth muscle actin (ACTA2)Smooth muscle myosin heavy chain (MYH11)Calponin (CNN1)Transgelin (SM22-alpha)

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